An efficient synthesis of SK-658 and its analogs as potent histone deacetylase inhibitors.

Md Shahidul Islam,Md Nurul Islam,Md Ashraful Hoque,Norikazu Nishino,Tamaki Kato,Hyun-Jung Kim,Akihiro Ito,Minoru Yoshida

Bioorganic chemistry（2015）

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摘要

SK-658 is a potent histone deacetylase (HDAC) inhibitor that showed higher activity than SAHA due to the presence of extended hydrophobic group. We designed and synthesized thioester and SS-hybrid bearing SK-658 analogs as HDAC inhibitors. All the compounds were active in nano molar range and showed higher inhibitory activity than SAHA and SK-658. Among these, disulfide compounds showed the highest activity.

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